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GW0742

CAS No. 317318-84-6

GW0742 ( GW0742 | GW-0742 | GW 0742 | GW0742X )

产品货号. M17477 CAS No. 317318-84-6

GW0742 (GW610742) 是一种有效且特异性的 PPARδ 激动剂(对于人 PPARδ/α/γ,EC50:1 nM/1.1 μM/2 μM)。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥348 有现货
10MG ¥551 有现货
25MG ¥1029 有现货
50MG ¥1871 有现货
100MG ¥3248 有现货
500MG ¥7719 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    GW0742
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    GW0742 (GW610742) 是一种有效且特异性的 PPARδ 激动剂(对于人 PPARδ/α/γ,EC50:1 nM/1.1 μM/2 μM)。
  • 产品描述
    GW0742, also known as GW610742 and GW0742X is a PPARδ/β agonist. GW0742 Induces Early Neuronal Maturation of Cortical Post-Mitotic Neurons. GW0742 prevents hypertension, vascular inflammatory and oxidative status, and endothelial dysfunction in diet-induced obesity. GW0742 has direct protective effects on right heart hypertrophy.GW0742 may enhance lipid metabolism in heart both in vivo and in vitro.
  • 体外实验
    GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ respectively. GW0742 (100 μM) activates human PPARα and mouse PPARβ in MCF-7 cells. GW0742 (100 μM) significantly reduces low-KCl-induced apoptosis of cerebellar granule neurons. GW0742 shows no obvious inherent toxicity on cerebellar granule neuronal cells after treatment of 3-100 μM for 24 h, but induces increased cell death at 100 μM after 48 hr of treatment. Moreover, GW0742 (100 μM) increases c-Jun expression in cerebellar granule neuron cultures observed at 6 hr. GW0742 (1 μM) induces PPARδ protein in neonatal rat cardiomyocytes. GW0742 also raises mRNA levels of long-chain acyl-CoA dehydrogenase (LCAD), very long-chain acyl-CoA dehydrogenase (VLCAD), acyl-CoA oxidase 1 (ACOX1), uncoupling protein 3 (UCP3), malonyl-CoA decarboxylase (MCD), and pyruvate dehydrogenase kinase 4 (PDK4) in neonatal rat cardiomyocytes.
  • 体内实验
    GW0742 (0.3 mg/kg, i.p.) reduces intensity masson-trichrome staining, and attenuates the histological signs in bleomycin instillatio (BLEO)-induced lung injury of mice. GW0742 (0.3 mg/kg, i.p.) also causes a reduction of the BLEO-induced loss body weight, and a decrease of myeloperoxidase (MPO) activity. GW0742 shows significant inhibition of TNF-a and IL-1β in instilled-mice. GW0742 prevents bleomycin-induced IkB-a degradation, reduces the levels of NF-kB p65 in the lung, and decreases iNOS and p-ERK expression in BLEO-induced mice. GW0742 (5 mg/kg/day, i.v.) increases PPARδ protein level in the heart of rats. GW0742 also induces the increase in LCAD, VLCAD, and ACOX1 in the heart of rats.
  • 同义词
    GW0742 | GW-0742 | GW 0742 | GW0742X
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    PPARδ|PPARα|PPARγ
  • 研究领域
    Metabolic Disease
  • 适应症
    ——

化学信息

  • CAS Number
    317318-84-6
  • 分子量
    471.49
  • 分子式
    C21H17F4NO3S2
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : ≥ 34 mg/mL; 72.11 mM
  • SMILES
    Cc1c(CSc2ccc(OCC(=O)O)c(C)c2)sc(n1)c1ccc(c(F)c1)C(F)(F)F
  • 化学全称
    [4-[[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methyl phenoxy]-acetic acid

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.Galuppo M, et al. GW0742, a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int J Immunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46.
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